Tramadol
Tramadol is a opioid that also acts as a SNRI. It is used as a prescription drug in many countries to treat moderate pain (often combined with paracetamol), and also sees recreational use for its euphoric effects. Due to its complex and atypical nature, it has also been investigated for use in the treatment of many conditions, including PTSD, opioid withdrawal, OCD and the management of diabetic side-effects.
History
Tramadol was first discovered in 1962 in Germany, and was later released under the brand name Tramal in 1977 - lauded due to its additional SNRI action. It later became a popular choice as a prescription drug for pain treatment around the world. Despite its branding and institutional view as a drug with little potential for abuse, it has increasing amounts of recreational use since release.
In 2013, it was discovered that tramadol is produced naturally in high concentrations in the root of the African pin cushion tree.
Dosage
Doses are given on a tolerance scale, since it accrues quickly; users should note that the lowering of the seizure threshold occurs regardless of tolerance.
No tolerance
Light: 50-100 mg
Common: 75 - 200 mg
Strong: 250+ mg
Common dosage with tolerance
Medium-High tolerance: 200-250 mg
Very High tolerance: 300-400 mg (Seizure threshold is dangerously lowered at this point.)
Extremely High tolerance: 400+ mg (Potentially fatal for new users. Seizure threshold is dangerously lowered at this point.)
Duration
Long onset, slowly building to a peak by hour 4 with maximum blood concentration achieved near hour 4.5.
Onset: 1-2 hours
Peak: 3-4 hours
Total Duration: 5-7 hours
Effects
Positive
- Euphoria
- Pain relief
- Elevated mood
- Overall feeling of contentedness
Neutral
- Itching
Negative
Some users may experience
- Nausea
- Constipation
- CNS depression
- Drowsiness
- Hot/cold flashes
- Dizziness
- Vomiting
- Urinary retention (difficulty urinating)
In high doses, overdoses, or in patients not tolerant to opiates, tramadol can cause shallow breathing, bradycardia, cold-clammy skin, apnea, hypotension, miosis, circulatory collapse, respiratory arrest, and death.
Chemistry and Pharmacology
Tramadol acts as a μ-opioid receptor agonist, serotonin releasing agent (SRA), serotonin and norepinephrine reuptake inhibitor (SNRI), NMDA receptor antagonist, 5-HT2C receptor antagonist, 5 nicotinic acetylcholine receptor antagonist,TRPV1 receptor agonist, and M1 and M3 muscarinic acetylcholine receptorantagonist. and can cause seizures, serotonin syndrome and even death when combined with certain stimulants and other reuptake inhibitors.
Harm Reduction
- Do not drive or operate machinery while under the influence of tramadol.
- Alcohol and many other drugs are extremely dangerous to combine with tramadol, for a list of interactions refer to Drug combinations.
- Tramadol effects serotonin levels in the brain. For this reason it is recommended to taper on, and taper off use.
Seizure Risk
We cannot stress this enough; if you have a history of seizures, we strongly urge you to stay away from tramadol as a recreational substance. By itself, it can decrease the seizure threshold. When combined with SSRIs, tricyclic antidepressants, or in patients with epilepsy, the seizure threshold is further decreased. Seizures have been reported in humans receiving excessive single oral doses (700 mg) or large intravenous doses (300 mg). However, there have been several rare cases of people having grand-mal seizures at doses as low as 100-400 mg orally.